PG-931 TFA

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PG-931 TFA;

PG-931 TFA 是 SHU 9119 (HY-P0227) 的类似物。PG-931 TFA 是一种强效的黑素皮质素 4 (MC4) 受体(IC50=0.58 nM) 激动剂，比 hMC3R (IC50=55 nM) 或 hMC5R (IC50=2.4 nM)更具选择性。PG-931 TFA 在动物实验模型中，可逆转出血休克，防止体内多器官损伤。

PG-931 TFAamp;;

PG-931 TFA Chemical Structure

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生物活性

PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo[2].

体内研究
(In Vivo)

PG-931 (intravenous injection; 13-108 nmol/kg; single dose) produces a dose-dependent restoration of cardiovascular and respiratory functions, and improved survival in Wistar rats with haemorrhagic shock[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats[1]
Dosage: 13-108 nmol/kg
Administration: Intravenous injection; single dose
Result: Exhibits an anti-shock effect occurred at nanomolar doses.

分子量

1294.42

Formula

C61H86F3N15O13
Sequence Shortening

Ac-{Nle}-DP-{D-Phe}-RWKPV-NH2 (Lactam bridge:Asp2-Lys7)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. D Giuliani, et al. Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br J Pharmacol

    [2]. P Grieco, et al. Extensive structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. J Pept Res